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24 Cards in this Set

  • Front
  • Back
List the cytotoxic drugs.
Azithioprine
Cyclosphosphoramide
List glucocorticoids (2)
Prednisone
Methylprednisone
Deflazacort
List calcineurin inhibitors
Cyclosporin
Tacrolimus
List immunosupprsesive antibodies
OKT3
Mechanism of azithioprine?

It is absorbed in?

Metabolized to?
Kill proliferating cells by inhibiting puring metabolism (DNA synthesis) during lymphoid cell proliferation after antigen stimulation. Both primary and 2ndary response is blocked.

GI

Mercaptopurine (purine analogue)
Clincal use of azithioprine?
1. inhibit immune response that causes rejection of kidney transplant
2. Severe rheumatoid arthritis (2nd choice)
3. Crohn's disease
4. Multiple Sclerosis
Side effects of azithioprine?
1. Leukopenia, anemia, thrombocytopenia --> susc to infection.
2. Nausea, vomiting, loss of appetite
3. Liver toxicity
(require regular blood count and liver function test)
To whom do you not give azithioprine to?why?

Others?
Pregnant - crosses placenta
Nursing mothers- found in milk

1. increase cancer risk
2. Impair fertility (reduce sperm count)
3. Increase toxicity with allopurinol
4. severe leukopenia when takin with ACE-I or bone marrow drugs
Mechanism of cyclophosphamide?
-Prodrug activated by P450 to 4-hydroxy-cyclophosphamide.
-Alkylating agent
-Cross linking DNA stands - inh antigen dependent proliferation of lymphocytes-> kill proliferating lymphocytes
Clinical use of cyclophosphamide?
1. SLE, Multiple sclerosis, Wegeners granulomatosis
2. Cancers: Leukemia, lymphoma, MM, mycosis fungoides, neuroblastoma, retinoblastoma, breast + ovary cancer
3. Immunosuppresive for organ transplant
Side effects of cyclosphosphamide?
Immediate:
1. nausea, vomiting
2. Cardiac toxicity
3. Electrolyte imbalance

Delayed:
1. Alopecia, hemorrhagic cystitis, risk of non-hodgkin lymphoma, bladder cancer, acute non-lymphoblastic leukemia, skin cancer
Mechanism of pnednisome?
1. Reduce size and #s of cells in lymph-node and spleen (no erythroid stem cells in Bone marrow)
2. Cytotoxic to subset of T cells. (mod of func, not cytotoxic)
3. inh production of leukotrienes, PGI, Histamine, bradykinin
4. attenuate chemotaxis, impair bacteriocidal and fungocidal activity of monocytes and neutrophils {no alteration of phagocytic activity}
6. Change leukocyte neutrophil distribution--> cells sequester in lymphoid tissue
7. Inh IL1 ---> low IL2, IFN-y production
8. reduce cellular and humoral immune response
Clinical use of prednisome?
1. Organ transplant, hematopoetic stem cell transplantation

a. allergic reactions bee stings, contact dermatitis, allergic drug reactions, allergic rhinitis
b. collagen-vascular disorders lupus erythematosus rheumatoid arthritis
c. eye disorders allergic conjunctivitis, optic neuritis
d. GI disorders inflammatory bowel disease
e. hematologic disorders and malignancies leukemia, autoimmune hemolytic anemia, multiple myeloma
f. Systemic inflammation acute respiratory distress syndrome, gram (-) septicemia to suppress excessive inflammation
h. joint inflammatory disorders arthritis, bursitits
i. neurlogical disorders cerebral edema (to minimize postoperative cerebral edema), multiple sclerosis
j. pulmonary disorders bronchial astma, infant respiratory distress syndrome
k. skin disorders dermatitis xerosis
Side effects of prednisone?

Other side effects include
1. peptic ulcers
2. masking the effects of bacterial and mycotic infections
3. nausea, dizziness and weight loss
4. hypomania or acurte psychosis (large doses)
5. increased intraocular pressure and glaucoma
6. impaired wound healing
1. Iatrogenic Cushing's syndrome (rounding and puffiness of the face (moon faces)).
2. redistribution of fat to the trunk and neck
3. increased growth of fine hair on face thichs and trunk
4. acne
5. insomnia
6. increased appetite
7. increased need for insulin with weight gain
8. development of insulin resistant diabetes.
Becareful when using prednisone for?
patients with peptic ulcer, heart disease of hypertension, psychosis, tuberculosis diabetes osteoporosis of glaucoma
Mech of methylprednisone?
It is a synthetic corticosteroid. MECH similar to prednisone
Clinical use of methylprednisome?
suppression of inflammatory conditions, including rheumatoid arthritis, systemic lupus erythematosus, acute gouty arthritis, psoriatic arthritis, ulcerative colitis, and Crohn's disease. Severe allergic conditions that fail to respond to conventional treatment may respond to methylprednisolone include; bronchial asthma, allergic rhinitis, drug-induced dermatitis, and contact and atopic dermatitis. Chronic skin conditions treated with methylprednisolone include dermatitis herpetiformis, pemphigus, severe psoriasis and severe seborrheic dermatitis. Chronic allergic and inflammatory conditions of the uvea, iris, conjunctiva and optic nerves of the eyes also are treated with methylprednisolone.
Side effects of methylprednisone depends on?
Dose, duration and frequency of admin.

Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, puffiness of the face, hair growth on the face, thinning and easy bruising of the skin, glaucoma, cataracts, peptic ulceration, worsening of diabetes, irregular menses, growth retardation in children, convulsions, and psychic disturbances. Psychic disturbances may include depression, euphoria, insomnia, mood swings, personality changes, and even psychotic behavior
Prolonged use of methylprednisolone can depress the ability of the body's adrenal glands to produce corticosteroids. Abruptly stopping methylprednisolone in these individuals can cause symptoms of corticosteroid insufficiency, with accompanying nausea, vomiting, and even shock. Therefore, withdrawal of methylprednisolone usually is accomplished by gradual tapering the dose. T/F
TRue

It's ok to give pregnant and nursing women.
Drug interactionS?
Troleandomycin-reduce liver's ability to metabolize methylprednisone (also other macrolides)

Birth control can increase the effect of corticosteroid by 50%

Phenobarbitol increase drug metabolism (need to increase dose)
Mech of deflazacort?
Drug used to decrease inflammation
Clinical use of deflazacort?
Control dz with excessive inflammation:
1. severe allergic rxn
2. inflammation of lung, asthma
3. inflammation of joins (arthritis)
4. Decrease white blood cells --> prevent rejection of transplants
5. Cancers : ALL, myelomas
6. SLE, rheumatoid arthritis
Side effects?
a) insomnia, b) depression, c) glaucoma, d) weight gain, e) irregular menstrual cycle, f) secreased functioning of the adrenal gland (adrenal suppression), g) thinning of the bones (osteoporosis), h) ulceration of the stomach or intestine, i) increased susceptibility to infections, j) acne, k) increased risk of fractures of the bones, l) increased hair growth (hirsutism), m) vaginal yeast infection (candidiasis), n) suppression of growth in children and adolescents and o) muscle wasting and weakness
D-D interactions?
Antifungal + oral contraceptive = increase effects of this drug

These increase remove of this drug:
antiepileptics (carbamazepine and phenytoi) and
barbituates (phenobarbitone) -
rifampicin
aminoglutethimide.

Antiacid-decrease absorption